BRPI0508481A - -substituted hydroxy-6-phenylenanthridines and their use as pde4 inhibitors - Google Patents

-substituted hydroxy-6-phenylenanthridines and their use as pde4 inhibitors

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Publication number
BRPI0508481A
BRPI0508481A BRPI0508481-4A BRPI0508481A BRPI0508481A BR PI0508481 A BRPI0508481 A BR PI0508481A BR PI0508481 A BRPI0508481 A BR PI0508481A BR PI0508481 A BRPI0508481 A BR PI0508481A
Authority
BR
Brazil
Prior art keywords
alkyl
alkoxy
hydrogen
pde4 inhibitors
fluorine
Prior art date
Application number
BRPI0508481-4A
Other languages
Portuguese (pt)
Inventor
Ulrich Kautz
Beate Schmidt
Dieter Flockerzi
Armin Hatzelmann
Christof Zitt
Johannes Barsig
Degenhard Marx
Hans-Peter Kley
Original Assignee
Altana Pharma Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Altana Pharma Ag filed Critical Altana Pharma Ag
Publication of BRPI0508481A publication Critical patent/BRPI0508481A/en

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    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C07D221/06—Ring systems of three rings
    • C07D221/10—Aza-phenanthrenes
    • C07D221/12—Phenanthridines
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/473—Quinolines; Isoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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Abstract

HIDRóXI-6-FENILENANTRIDINAS AMIDO-SUBSTITUìDAS E SEU USO COMO INIBIDORES DA PDE4. A patente de invenção refere-se a compostos de fórmula (I) na qual, R1 é hidroxila, alcóxi C1-4, cicloalcóxi C3-7, cicloalquilmetóxi C3-7, 2,2-difluoretóxi ou alcóxi C1-4 completamente ou predominantemente substituído por flúor, R2 é hidroxila, alcóxi C1-4, cicloalcóxi C3-7, cicloalquilmetóxi C3-7, 2,2-difluoretóxi ou alcóxi C1-4 completamente ou predominantemente substituído por flúor, ou na qual R1 e R2 juntos são um grupo alquilenodióxi C1-2, R3 é hidrogênio ou alquila C1-4, R31 é hidrogênio ou alquila C1-4, um ou outro, em uma primeira modalidade (modalidade a) de acordo com a presente invenção, R4 é -O-R41, no qual R41 é hidrogênio, alquila C1-4, alcóxi C1-4-alquila C1-4, hidroxialquila C2-4, alquilcarbonila C1-7 ou aquila C1-4 completamente ou predominantemente substituída por flúor, e R5 é hidrogênio ou alquila C1-4 ou, em uma segunda modalidade (modalidade b) de acordo com a presente invenção, R4 é hidrogênio ou alquila C1-4, e R5 é -O- R51, no qual R51 é hidrogênio, alquila C1-4, alcóxi C1-4-alquila C1-4, hidroxialquila C2-4, alquilcarbonila C1-7 ou alquila C1-4 completamente ou predominantemente substituída por flúor, R6 é hidrogênio, halogênio, alquila C1-4 ou alcóxi C1-4, um ou outro, em um primeiro aspecto (aspecto 1) de acordo com a presente invenção, R7 é -N(R8)R9 ou, em um segundo aspecto (aspecto 2) de acordo com a presente invenção, R7 é -NH-N(R18)R19, são novos inibidores eficazes da PDE4.HYDROXY-6-PHENYLENANTHRIDINES, starch-substituted and their use as PDE4 inhibitors. The patent relates to compounds of formula (I) wherein R1 is hydroxyl, C1-4 alkoxy, C3-7 cycloalkoxy, C3-7 cycloalkylmethoxy or fully or predominantly substituted C1-4 alkoxy by fluorine, R2 is hydroxyl, C1-4 alkoxy, C3-7 cycloalkoxy, C3-7 cycloalkylmethoxy, 2,2-difluorooxy or C1-4 alkoxy completely or predominantly substituted by fluorine, or wherein R1 and R2 together are an alkylenedioxy group C1-2, R3 is hydrogen or C1-4 alkyl, R31 is hydrogen or C1-4 alkyl, either, in a first embodiment (embodiment a) according to the present invention, R4 is -O-R41, in which R41 is hydrogen, C1-4 alkyl, C1-4 alkoxy-C1-4 alkyl, C2-4 hydroxyalkyl, C1-7 alkylcarbonyl or C1-4 alkyl completely or predominantly substituted by fluorine, and R5 is hydrogen or C1-4 alkyl or , in a second embodiment (embodiment b) according to the present invention, R 4 is hydrogen or C 1-4 alkyl, and R 5 is -O- R 51, wherein R51 is hydrogen, C1-4 alkyl, C1-4 alkoxy-C1-4 alkyl, C2-4 hydroxyalkyl, C1-7 alkylcarbonyl or C1-4 alkyl completely or predominantly substituted by fluorine, R6 is hydrogen, halogen, C1-4 alkyl or C1-4 alkoxy, either, in a first aspect (aspect 1) according to the present invention, R7 is -N (R8) R9 or, in a second aspect (aspect 2) according to the present invention, R7 is -NH-N (R18) R19, are new effective PDE4 inhibitors.

BRPI0508481-4A 2004-03-10 2005-03-09 -substituted hydroxy-6-phenylenanthridines and their use as pde4 inhibitors BRPI0508481A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP04100990 2004-03-10
EP04106677 2004-12-17
PCT/EP2005/051054 WO2005087745A1 (en) 2004-03-10 2005-03-09 Novel amido-substituted hydroxy-6-phenylphenanthridines and their use as pde4 inhibitors

Publications (1)

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BRPI0508481A true BRPI0508481A (en) 2007-07-31

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US (1) US20070185149A1 (en)
EP (1) EP1725534A1 (en)
JP (1) JP2007527901A (en)
KR (1) KR20060130697A (en)
CN (1) CN1926113B (en)
AR (1) AR049324A1 (en)
AU (1) AU2005221832A1 (en)
BR (1) BRPI0508481A (en)
CA (1) CA2558391A1 (en)
IL (1) IL177496A0 (en)
MX (1) MXPA06009892A (en)
NO (1) NO20064415L (en)
NZ (1) NZ549254A (en)
TW (1) TW200600499A (en)
WO (1) WO2005087745A1 (en)

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CA2558391A1 (en) 2005-09-22
CN1926113A (en) 2007-03-07
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AR049324A1 (en) 2006-07-19
WO2005087745A1 (en) 2005-09-22
JP2007527901A (en) 2007-10-04
US20070185149A1 (en) 2007-08-09
MXPA06009892A (en) 2007-03-01
AU2005221832A1 (en) 2005-09-22
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IL177496A0 (en) 2006-12-10
TW200600499A (en) 2006-01-01

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